Home Metabolism PDE inhibitor Udenafil For research use only.

Udenafil

Udenafil is a potent antagonist of human PDE5 with an IC50 of 8.25 nM and a comparable selectivity profile as sildenafil for the other PDEs.

Udenafil Chemical Structure

Udenafil Chemical Structure

CAS: 268203-93-6

Purity & Quality Control

Batch: S643301 DMSO] 100 mg/mL] false] Ethanol] 25 mg/mL] false] Water] Insoluble] false Purity: 99.99%
99.99

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Signaling Pathway

PDE Signaling Pathways

PDE Signaling Pathway

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Biological Activity

Description Udenafil is a potent antagonist of human PDE5 with an IC50 of 8.25 nM and a comparable selectivity profile as sildenafil for the other PDEs.
Targets
PDE5 [1]
(Cell-free assay)		 PDE3 [1]
(Cell-free assay)		 PDE6 [1]
(Cell-free assay)		 PDE2 [1]
(Cell-free assay)
8.25 nM 52 nM 53.3 nM 101 nM
In vitro
In vitro

The inhibitory effect of udenafil on PDE5 is about 150-fold greater than that on PDE1 (selectivity ratio of 149). PDE11 selectivity of udenafil (selectivity ratio of 96) is relatively high, indicating a very low probability of inhibition of PDE11 at therapeutic doses of udenafil. The IC50 values for PDE2, PDE3, and PDE6 of udenafil are 101±15.1 nM, 52.0±3.53 nM, and 53.3±2.47 nM respectively[1].
In Vivo
In vivo

Udenafil is rapidly absorbed, reaching peak plasma concentrations at 0.8-1.3 h, then declining monoexponentially with a terminal half-life (T1/2) between 7.3 and 12.1 hours, giving it the unique pharmacokinetics of both relatively rapid onset and long duration. Udenafil has also been shown in preclinical studies to have potent erectogenic properties in rats and rabbits with a broad safety margin[2]. Absolute oral bioavailability of udenafil is only 38% in rats. This low oral bioavailability of udenafil appears to be mainly due to a considerable intestinal first-pass effect[1].
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01928563 Unknown status
Healthy Male Subjects
Dong-A Pharmaceutical Co. Ltd.|Dong-A ST Co. Ltd.
 September 2013 Phase 1
NCT01929213 Unknown status
Healthy Volunteers
Dong-A Pharmaceutical Co. Ltd.|Dong-A ST Co. Ltd.
 August 2013 Phase 1
NCT01108900 Completed
Erectile Dysfunction
Pfizer''s Upjohn has merged with Mylan to form Viatris Inc.|Pfizer
 July 2010 --

Chemical Information & Solubility

Molecular Weight 516.66 Formula

C25H36N6O4S
CAS No. 268203-93-6 SDF --
Smiles CCCC1=NN(C2=C1N=C(NC2=O)C3=C(C=CC(=C3)S(=O)(=O)NCCC4CCCN4C)OCCC)C
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (193.55 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 25 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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